Tamatinib besylate (R406)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
Size | Price | Stock |
---|---|---|
250mg | $1080 | Check With Us |
500mg | $1620 | Check With Us |
1g | $2430 | Check With Us |
Cat #: V0583 CAS #: 841290-81-1 Purity ≥ 98%
Description: Tamatinib besylate (formerly R-406 besylate; prodrug of R 406) is a novel, potent and ATP-competitive inhibitor of spleen tyrosine kinase/Syk with potential anti-inflammatory activity.
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Molecular Weight (MW) | 628.63 |
---|---|
Molecular Formula | C22H23FN6O5.C6H6O3S |
CAS No. | 841290-81-1 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 126 mg/mL (200.4 mM)r |
Water: <1 mg/mLr | |
Ethanol: 8 mg/mL (12.7 mM) | |
Solubility In Vivo | 30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL |
SMILES Code | CC1(C(=O)NC2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)C.C1=CC=C(C=C1)S(=O)(=O)O |
Synonyms | R406 benzenesulfonate; R-406 benzenesulfonate; R-406 besylate; R406; R-406; R 406; R 406 besylate; R406 besylate; R406 benzenesulfonate; Tamatinib, |
Protocol | In Vitro | R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells. R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 µM, respectively. R406 inhibits adenosine A3 receptor (IC50=0.081 µM), adenosine transporter (IC50=1.84 µM), and monoamine transporter (IC50=2.74 µM). |
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In Vivo | R406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.5908 mL | 7.9538 mL | 15.9076 mL | 31.8152 mL |
5mM | 0.3182 mL | 1.5908 mL | 3.1815 mL | 6.3630 mL |
10mM | 0.1591 mL | 0.7954 mL | 1.5908 mL | 3.1815 mL |
20mM | 0.0795 mL | 0.3977 mL | 0.7954 mL | 1.5908 mL |
The molarity calculator equation
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The dilution calculator equation
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.